Synthesis and evaluation of water-soluble polymeric bone-targeted drug delivery systems

Bioconjug Chem. 2003 Sep-Oct;14(5):853-9. doi: 10.1021/bc034090j.

Abstract

Four polymeric bone-targeting conjugates were synthesized based on poly(ethylene glycol) (PEG, two conjugates) and poly[N-(2-hydroxypropyl)methacrylamide] (PHPMA, two conjugates). The well-known bone-targeting compounds, alendronate and aspartic acid peptide, were used as bone-targeting moieties. Fluorescein isothiocyanate (FITC) was attached to the conjugates as a model drug for detection purposes. The bone-targeting potential of these conjugates was tested in vitro with hydroxyapatite (HA) and in mice. The data obtained indicated that these novel delivery systems could specifically accumulate in the bone tissue.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Alendronate / chemical synthesis
  • Alendronate / metabolism
  • Animals
  • Binding Sites / physiology
  • Bone and Bones / drug effects
  • Bone and Bones / metabolism*
  • D-Aspartic Acid / chemical synthesis
  • D-Aspartic Acid / metabolism
  • Drug Delivery Systems / methods*
  • Drug Evaluation, Preclinical / methods
  • Male
  • Mice
  • Mice, Inbred BALB C
  • Polymers / administration & dosage
  • Polymers / chemical synthesis*
  • Polymers / metabolism*
  • Solubility
  • Water / chemistry
  • Water / metabolism

Substances

  • Polymers
  • Water
  • D-Aspartic Acid
  • Alendronate